Supplementary material from "Pyrazole-based inhibitors of enhancer of zeste homologue 2 induce apoptosis and autophagy in cancer cells"
Posted on 2018-03-07 - 18:14
Novel pyrazole-based EZH2 inhibitors have been prepared through a molecular pruning approach from known inhibitors bearing a bicyclic moiety as a central scaffold. The hit compound 1o [N-((4,6-dimethyl-2-oxo-1,2-dihydropyridin-3-yl)methyl)-5-methyl-1-phenyl-1H-pyrazole-4-carboxamide] showed low micromolar EZH2/PRC2 inhibition and high selectivity towards a panel of other methyltransferases. Moreover, 1o displayed cell growth arrest in breast MDA-MB231, leukaemia K562, and neuroblastoma SK-N-BE cancer cells joined to reduction of H3K27me3 levels and induction of apoptosis and autophagy.This article is part of a discussion meeting issue ‘Frontiers in epigenetic chemical biology’.
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Mellini, Paolo; Marrocco, Biagina; Borovika, Diana; Polletta, Lucia; Carnevale, Ilaria; Saladini, Serena; et al. (2018). Supplementary material from "Pyrazole-based inhibitors of enhancer of zeste homologue 2 induce apoptosis and autophagy in cancer cells". The Royal Society. Collection. https://doi.org/10.6084/m9.figshare.c.4025029.v1
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AUTHORS (13)
PM
Paolo Mellini
BM
Biagina Marrocco
DB
Diana Borovika
LP
Lucia Polletta
IC
Ilaria Carnevale
SS
Serena Saladini
GS
Giulia Stazi
CZ
Clemens Zwergel
PT
Peteris Trapencieris
EF
Elisabetta Ferretti
MT
Marco Tafani
SV
Sergio Valente
AM
Antonello Mai